ES2121223T3 - Derivados de indol como antagonistas de tromboxano a2. - Google Patents

Derivados de indol como antagonistas de tromboxano a2.

Info

Publication number
ES2121223T3
ES2121223T3 ES94924864T ES94924864T ES2121223T3 ES 2121223 T3 ES2121223 T3 ES 2121223T3 ES 94924864 T ES94924864 T ES 94924864T ES 94924864 T ES94924864 T ES 94924864T ES 2121223 T3 ES2121223 T3 ES 2121223T3
Authority
ES
Spain
Prior art keywords
alkyl
pct
imidazolyl
pyridyl
cycloalkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
ES94924864T
Other languages
English (en)
Inventor
Peter Edward Cross
Kevin Neil Dack
Roger Peter Dickinson
John Steele
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pfizer Research and Development Co NV SA
Original Assignee
Pfizer Research and Development Co NV SA
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pfizer Research and Development Co NV SA filed Critical Pfizer Research and Development Co NV SA
Application granted granted Critical
Publication of ES2121223T3 publication Critical patent/ES2121223T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

COMPUESTOS DE LA FORMULA (I) Y LAS SALES FARMACEUTICAMENTE ACEPTABLES Y ESTERES BIOLABILES DE LOS MISMOS, EN LA QUE R{SUP,1} ES H, ALQUILO C{SUB,1}-C{SUB,4}, FENILO OPCIONALMENTE SUSTITUIDO POR HASTA TRES SUSTITUYENTES INDEPENDIENTEMENTE SELECCIONADOS DEL ALQUILO C{SUB,1}-C{SUB,4}, ALCOXI C{SUB,1}-C{SUB,4}, HALOGENO Y CF{SUB,3}, O ES 1-IMIDAZOLILO, 3-PIRIDILO O 4-PIRIDILO, R{SUP,2} ES H O ALQUILO C{SUB,1}-C{SUB,4}, R{SUP,3} ES SO{SUB,2}R{SUP,4} O COR{SUP,4} DONDE R{SUP,4} ES ALQUILO C{SUB,1}-C{SUB,6}, PERFLUORALQUIL(CH{SUB,2}){SUB,P} C{SUB,1}-C{SUB,3}, CICLOALQUIL(CH{SUB,2}){SUB,P} C{SUB,3}-C{SUB,6}, ARIL(CH{SUB,2}){SUB,P} O HETEROARIL(CH{SUB,2}){SUB,P}, DONDE P ES 0, 1 O 2, O R{SUP,4} PUEDE SER NR{SUP,5}R{SUP,6} DONDE R{SUP,5} ES H O ALQUILO C{SUB,1}-C{SUB,4} Y R{SUP,6} ES ALQUILO C{SUB,1}-C{SUB,6}, CICLOALQUILO C{SUB,3}-C{SUB,6} O ARILO, O R{SUP,5} Y R{SUP,6} JUNTO CON EL ATOMO DE NITROGENO AL QUE ESTA UNIDOS FORMAN UN ANILLO HETEROCICLICO DE 5 A 7 ELEMENTOS QUE PUEDEN INCORPORAR OPCIONALMENTE UN DOBLE ENLACE CARBONO-CARBONO U OTRO ENLACE MAS DE UN HETEROATOMO SELECCIONADO DEL O, S, NH, N(ALQUILO C{SUB,1}-C{SUB,4}) Y N(ALCANOILO C{SUB,1}-C{SUB,5}); X ES CH{SUB,2} O UN ENLACE DIRECTO, CON LA CONDICION DE QUE CUANDO R{SUP,1} SEA 1-IMIDAZOLILO X SEA ENTONCES CH{SUB,2}; M ES 2 O 3; N ES 0, 1 O 2 Y EN DONDE EL GRUPO (CH{SUB,2}){SUB,N}NHR{SUP,3} SE ENCUENTRA ACOPLADO EN LA POSICION 5 CUANDO N ES 0 O 1, O EN LA POSICION 5 O 4 CUANDO N ES 2. ESTOS COMPUESTOS SON ANTAGONISTAS SELECTIVOS DEL TXA{SUB,2} Y DEL PGH{SUB,2}. ALGUNOS TAMBIEN INHIBEN LA SINTETASA DE TROMBOXANO.
ES94924864T 1993-08-26 1994-08-09 Derivados de indol como antagonistas de tromboxano a2. Expired - Lifetime ES2121223T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB939317764A GB9317764D0 (en) 1993-08-26 1993-08-26 Therapeutic compound

Publications (1)

Publication Number Publication Date
ES2121223T3 true ES2121223T3 (es) 1998-11-16

Family

ID=10741074

Family Applications (1)

Application Number Title Priority Date Filing Date
ES94924864T Expired - Lifetime ES2121223T3 (es) 1993-08-26 1994-08-09 Derivados de indol como antagonistas de tromboxano a2.

Country Status (11)

Country Link
US (1) US5744488A (es)
EP (1) EP0715627B1 (es)
JP (1) JP2763962B2 (es)
AT (1) ATE170856T1 (es)
CA (1) CA2170279A1 (es)
DE (1) DE69413238T2 (es)
DK (1) DK0715627T3 (es)
ES (1) ES2121223T3 (es)
FI (1) FI960840A (es)
GB (1) GB9317764D0 (es)
WO (1) WO1995006046A1 (es)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2222829A1 (es) * 2003-07-30 2005-02-01 Laboratorios Del Dr. Esteve, S.A. Derivados de 4-indolilsulfonamidas, su preparacion y su aplicacion como medicamentos.
ES2222827A1 (es) * 2003-07-30 2005-02-01 Laboratorios Del Dr. Esteve, S.A. Derivados de 5-indolilsulfonamidas, su preparacion y su aplicacion como medicamentos.

Families Citing this family (44)

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CA2317439A1 (en) 1998-01-14 1999-07-22 Wayne J. Brouillette Methods of synthesizing and screening inhibitors of bacterial nad synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial nad synthetase enzyme
US6861448B2 (en) * 1998-01-14 2005-03-01 Virtual Drug Development, Inc. NAD synthetase inhibitors and uses thereof
US6673827B1 (en) 1999-06-29 2004-01-06 The Uab Research Foundation Methods of treating fungal infections with inhibitors of NAD synthetase enzyme
MXPA02003122A (es) * 1998-03-31 2004-04-21 Inst For Pharm Discovery Inc Acidos indolalcanoicos substituidos.
TNSN99224A1 (fr) * 1998-12-01 2005-11-10 Inst For Pharm Discovery Inc Methodes de reduction des niveaux de glucose et triglyceride en serum et pour suppression de l'antigenese utilisant les acides la indolealkanoique
US6663862B1 (en) * 1999-06-04 2003-12-16 Duke University Reagents for detection and purification of antibody fragments
GB0010757D0 (en) 2000-05-05 2000-06-28 Astrazeneca Ab Chemical compounds
CA2436130A1 (en) * 2001-01-29 2002-08-08 3-Dimensional Pharmaceuticals, Inc. Substituted indoles and their use as integrin antagonists
US6872730B2 (en) * 2001-04-27 2005-03-29 3-Dimensional Pharmaceuticals, Inc. Substituted benzofurans and benzothiophenes, methods of making and methods of use as integrin antagonists
FR2827287B1 (fr) * 2001-07-13 2003-10-31 Servier Lab Nouveaux derives de benzene sulfonamide, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
GB0121941D0 (en) 2001-09-11 2001-10-31 Astrazeneca Ab Chemical compounds
AU2003256926A1 (en) * 2002-07-26 2004-02-16 The Institutes For Pharmaceutical Discovery, Llc Substituted indolealkanoic acids derivative and formulations containing same for use in treatment of diabetic complications
US7442805B2 (en) 2003-09-25 2008-10-28 Wyeth Substituted sulfonamide-indoles
GB0324763D0 (en) 2003-10-23 2003-11-26 Oxagen Ltd Use of compounds in therapy
HN2004000536A (es) 2003-12-16 2009-02-18 Wyeth Corp Un procediemiento de sintesis para la alquilacion reductiva de la posicon c-3 de indoles
US7714017B2 (en) * 2004-10-12 2010-05-11 Decode Genetics, Ehf Carboxylic acid peri-substituted bicyclics for occlusive artery disease
AU2006279496A1 (en) 2005-08-17 2007-02-22 Wyeth Substituted indoles and use thereof
ATE517883T1 (de) * 2005-08-25 2011-08-15 Schering Corp Imidazolderivate als funktionelle selektive agonisten des alpha2c-adrenorezeptors
ES2439736T3 (es) 2005-11-08 2014-01-24 Vertex Pharmaceuticals Incorporated Moduladores heterocíclicos de transportadores de casete de unión a ATP
US7671221B2 (en) 2005-12-28 2010-03-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
US7932284B2 (en) * 2006-01-24 2011-04-26 Eli Lilly And Company Indole sulfonamide modulators of progesterone receptors
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
RU2451018C2 (ru) 2006-04-07 2012-05-20 Вертекс Фармасьютикалз Инкорпорейтед Модуляторы атф-связывающих кассетных транспортеров
US7645789B2 (en) 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US7754739B2 (en) 2007-05-09 2010-07-13 Vertex Pharmaceuticals Incorporated Modulators of CFTR
KR20090125799A (ko) * 2007-03-29 2009-12-07 아스비오파마 가부시키가이샤 Ｃｐｌａ2 저해 활성을 가지는 인돌 유도체 및 그 용도 및 제조 방법
CN104447716A (zh) 2007-05-09 2015-03-25 沃泰克斯药物股份有限公司 Cftr调节剂
CN101910156B (zh) 2007-12-07 2013-12-04 沃泰克斯药物股份有限公司 3-(6-(1-(2,2-二氟苯并[d][1,3]间二氧杂环戊烯-5-基)环丙烷甲酰氨基)-3-甲基吡啶-2-基)苯甲酸的固体形式
CA2989620C (en) 2007-12-07 2022-05-03 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
US7750027B2 (en) * 2008-01-18 2010-07-06 Oxagen Limited Compounds having CRTH2 antagonist activity
EP2271622B1 (en) 2008-02-28 2017-10-04 Vertex Pharmaceuticals Incorporated Heteroaryl derivatives as CFTR Modulators
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
DK3150198T3 (da) 2010-04-07 2021-11-01 Vertex Pharma Farmaceutiske sammensætninger af 3-(6-(1-(2,2-difluorbenzo[d][1,3]dioxol-5-yl)-cyclopropancarboxamido)-3-methylpyriodin-2-yl)benzoesyre og indgivelse deraf
MX2012012204A (es) 2010-04-22 2012-12-05 Vertex Pharma Proceso para producir compuestos de cicloalquilcarboxamido-indol.
CA2819373A1 (en) 2010-12-09 2012-06-14 Amgen Inc. Bicyclic compounds as pim inhibitors
US9321756B2 (en) 2011-03-22 2016-04-26 Amgen Inc. Azole compounds as PIM inhibitors
AR092857A1 (es) 2012-07-16 2015-05-06 Vertex Pharma Composiciones farmaceuticas de (r)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-il)-n-(1-(2,3-dihidroxipropil)-6-fluoro-2-(1-hidroxi-2-metilpropan-2-il)-1h-indol-5-il)ciclopropancarboxamida y administracion de las mismas
US10231932B2 (en) 2013-11-12 2019-03-19 Vertex Pharmaceuticals Incorporated Process of preparing pharmaceutical compositions for the treatment of CFTR mediated diseases
GB201322273D0 (en) 2013-12-17 2014-01-29 Atopix Therapeutics Ltd Process
ES2957761T3 (es) 2014-04-15 2024-01-25 Vertex Pharma Composiciones farmacéuticas para el tratamiento de enfermedades mediadas por el regulador de la conductancia transmembrana de fibrosis quística
GB201407807D0 (en) 2014-05-02 2014-06-18 Atopix Therapeutics Ltd Polymorphic form
GB201407820D0 (en) 2014-05-02 2014-06-18 Atopix Therapeutics Ltd Polymorphic form
JP6494757B2 (ja) 2014-11-18 2019-04-03 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ ハイスループット試験高速液体クロマトグラフィーを行うプロセス

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2045244B (en) * 1979-03-07 1983-01-26 Pfizer Ltd 3-1-(imidazolylalkyl) indoles
ZA825413B (en) * 1981-08-26 1983-06-29 Pfizer Thromboxane synthetase inhibitors, processes for their production, and pharmaceutical compositions comprising them
US4474967A (en) * 1983-04-27 1984-10-02 Pfizer Inc. 8-Deutero and 8-tritio-substituted derivatives of D-4S-6-fluoro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2222829A1 (es) * 2003-07-30 2005-02-01 Laboratorios Del Dr. Esteve, S.A. Derivados de 4-indolilsulfonamidas, su preparacion y su aplicacion como medicamentos.
ES2222827A1 (es) * 2003-07-30 2005-02-01 Laboratorios Del Dr. Esteve, S.A. Derivados de 5-indolilsulfonamidas, su preparacion y su aplicacion como medicamentos.
US8097643B2 (en) 2003-07-30 2012-01-17 Laboratorios Del Dr. Esteve S. A. Indol-4 sulfonamide derivatives, their preparation and their use 5-ht-6 as modulators

Also Published As

Publication number Publication date
FI960840A0 (fi) 1996-02-23
ATE170856T1 (de) 1998-09-15
CA2170279A1 (en) 1995-03-02
JPH08509003A (ja) 1996-09-24
US5744488A (en) 1998-04-28
DE69413238D1 (en) 1998-10-15
DE69413238T2 (de) 1999-01-28
FI960840A (fi) 1996-02-23
EP0715627B1 (en) 1998-09-09
DK0715627T3 (da) 1999-06-07
JP2763962B2 (ja) 1998-06-11
EP0715627A1 (en) 1996-06-12
GB9317764D0 (en) 1993-10-13
WO1995006046A1 (en) 1995-03-02

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